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CA2371972A1 - Ent-steroids as selectively active estrogens - Google Patents

Ent-steroids as selectively active estrogens Download PDF

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Publication number
CA2371972A1
CA2371972A1 CA002371972A CA2371972A CA2371972A1 CA 2371972 A1 CA2371972 A1 CA 2371972A1 CA 002371972 A CA002371972 A CA 002371972A CA 2371972 A CA2371972 A CA 2371972A CA 2371972 A1 CA2371972 A1 CA 2371972A1
Authority
CA
Canada
Prior art keywords
ent
estra
beta
alpha
diol
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Abandoned
Application number
CA002371972A
Other languages
English (en)
French (fr)
Inventor
Sigfrid Schwarz
Dirk Kosemund
Gerd Muller
Margit Richter
Olaf Peters
Peter Droescher
Walter Elger
Alexander Hillisch
Ulf Bomer
Karl-Heinrich Fritzemeier
Christa Hegele-Hartung
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Bayer Pharma AG
Original Assignee
Individual
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Individual filed Critical Individual
Publication of CA2371972A1 publication Critical patent/CA2371972A1/en
Abandoned legal-status Critical Current

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • A61K31/566Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol having an oxo group in position 17, e.g. estrone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • A61K31/567Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in position 17 alpha, e.g. mestranol, norethandrolone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/02Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10Drugs for genital or sexual disorders; Contraceptives for impotence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/12Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/30Oestrogens
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/32Antioestrogens
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/14Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Gynecology & Obstetrics (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Pregnancy & Childbirth (AREA)
  • Psychiatry (AREA)
  • Immunology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
CA002371972A 1999-04-15 2000-04-17 Ent-steroids as selectively active estrogens Abandoned CA2371972A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DE19917930A DE19917930A1 (de) 1999-04-15 1999-04-15 Ent-Steroide als selektiv wirksame Estrogene
DE19917930.1 1999-04-15
PCT/EP2000/003470 WO2000063228A1 (en) 1999-04-15 2000-04-17 Ent-steroids as selectively active estrogens

Publications (1)

Publication Number Publication Date
CA2371972A1 true CA2371972A1 (en) 2000-10-26

Family

ID=7905255

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002371972A Abandoned CA2371972A1 (en) 1999-04-15 2000-04-17 Ent-steroids as selectively active estrogens

Country Status (11)

Country Link
EP (1) EP1169336B1 (es)
JP (1) JP2002542255A (es)
AR (1) AR023497A1 (es)
AT (1) ATE316978T1 (es)
AU (1) AU4401100A (es)
CA (1) CA2371972A1 (es)
CO (1) CO5180552A1 (es)
DE (2) DE19917930A1 (es)
ES (1) ES2258005T3 (es)
PE (1) PE20010042A1 (es)
WO (1) WO2000063228A1 (es)

Families Citing this family (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6350739B1 (en) 1999-08-11 2002-02-26 University Of Florida Resarch Foundation, Inc. Methods of prevention and treatment of ischemic damage
US6958327B1 (en) 1999-11-02 2005-10-25 Schering, Ag 18 Norsteroids as selectively active estrogens
DE50014299D1 (de) * 1999-11-02 2007-06-14 Bayer Schering Pharma Ag 18-nor-steroide als selektiv wirksame estrogene
DE10039199A1 (de) * 2000-08-10 2002-02-21 Schering Ag Kombinationspräparate aus einem ERß selektiven Estrogen und einem SERM oder Antiestrogen
GB0020498D0 (en) * 2000-08-18 2000-10-11 Sterix Ltd Compound
DE10048634A1 (de) * 2000-09-27 2002-04-18 Jenapharm Gmbh 19-Nor-17alpha-pregna-1,3,5(10)-trien-17beta-ole mit einem 21, 16alpha-Laktonring
CA2427817C (en) 2000-11-03 2009-04-14 Washington University Estrone-derivatives having cytoprotective activity
US20020132802A1 (en) * 2000-11-17 2002-09-19 Washington Univeristy Cytoprotective polycyclic compounds
DK1365768T3 (da) * 2001-02-27 2008-08-18 Bayer Schering Pharma Ag Anvendelse af ER-beta-selektive antagonister som contraception.
DE10151365A1 (de) 2001-10-17 2003-04-30 Schering Ag 17-Chlor-D-Homosteroide als selektive Estrogenrezeptorantagonisten
DK1390040T3 (da) 2001-05-18 2007-04-23 Pantarhei Bioscience Bv Farmaceutisk præparat til anvendelse i hormonerstatningsterapi
DE60223795T2 (de) 2001-05-23 2008-11-27 Pantarhei Bioscience B.V. Tetrahydroxyliertes Östrogen enthaltendes Arzneistoffverabreichungssystem zur Verwendung in der hormonalen Kontrazeption
US7871995B2 (en) 2001-05-23 2011-01-18 Pantarhei Bioscience B.V. Drug delivery system comprising a tetrahydroxylated estrogen for use in hormonal contraception
DE10151363A1 (de) * 2001-10-17 2003-05-08 Schering Ag Somatotrope Therapie
EP1446128B1 (en) 2001-11-15 2006-12-06 Pantarhei Bioscience B.V. Use of estrogenic compounds in combination with progestogenic compounds in hormone-replacement therapy
EP1358882A1 (en) * 2002-04-30 2003-11-05 Schering Aktiengesellschaft Use of estriol sulfamate prodrugs for the treatment of autoimmune diseases
EP1511498B1 (en) 2002-06-11 2012-11-21 Pantarhei Bioscience B.V. A method of treating human skin and a skin care composition for use in such a method
WO2003103684A1 (en) 2002-06-11 2003-12-18 Pantarhei Bioscience B.V. Method of treating or preventing immune mediated disorders and pharmaceutical formulation for use therein
SI1526856T1 (sl) 2002-07-12 2008-04-30 Pantarhei Bioscience Bv Farmacevtski sestavek, ki obsega estetrolne derivate za uporabo pri zdravljenju raka
ATE410170T1 (de) * 2003-03-27 2008-10-15 Pantarhei Bioscience Bv Verwendung von estrogenen zur behandlung von männerunfruchtbarkeit
DE10317922B4 (de) * 2003-04-17 2009-11-26 Presearch Gmbh Verwendung eines Kombinationspräparates aus oralem Kontrazeptivum und Calcium/Vitamin D
US8236785B2 (en) 2007-01-08 2012-08-07 Pantarhei Bioscience B.V. Method of treating or preventing infertility in a female mammal and pharmaceutical kit for use in such method
ES2310968B1 (es) * 2007-06-25 2010-02-08 Italfarmaco, S.A. Uso de estriol en bajas dosis.
CA2729635A1 (en) * 2008-07-03 2010-01-07 Ananth Srinivasan Compounds and processes for production of radiopharmaceuticals
BR112014005373B1 (pt) 2011-09-08 2022-04-19 Sage Therapeutics, Inc Compostos esteróides neuroativos, composições e usos destes
IL280068B1 (en) 2013-03-13 2025-02-01 Sage Therapeutics Inc Neuroactivity is modulated at position 24 by hydroxy and alkyl/alkenyl/alkynyl 3beta–hydroxy–cholane and 3beta–hydroxy–chol–5–ene derivatives
JP6628745B2 (ja) 2014-06-18 2020-01-15 セージ セラピューティクス, インコーポレイテッド オキシステロールおよびその使用方法
CN104926916B (zh) * 2015-06-05 2016-08-24 郑祖兰 甾体化合物,含其药物组合物及其制备方法和应用
PT3436022T (pt) 2016-04-01 2022-07-04 Sage Therapeutics Inc Oxisteróis e métodos de utilização dos mesmos
WO2017193046A1 (en) 2016-05-06 2017-11-09 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
TWI752976B (zh) 2016-07-07 2022-01-21 美商賽吉醫療公司 氧固醇(oxysterol)及其使用方法
PT3519422T (pt) 2016-09-30 2022-12-05 Sage Therapeutics Inc Oxisteróis substituídos em c7 e métodos como moduladores nmda
EP4105223A1 (en) 2016-10-18 2022-12-21 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
EP4034618A1 (en) 2019-09-27 2022-08-03 Basf Se Process for the purification of phytosterol

Family Cites Families (10)

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Publication number Priority date Publication date Assignee Title
FR1453212A (fr) * 1963-06-05 1966-06-03 Roussel Uclaf Dérivés stéroïdes et procédé de préparation
GB1103871A (en) * 1964-03-11 1968-02-21 Emi Ltd Improvements relating to magnetic matrix stores
FR1509931A (fr) * 1966-04-29 1968-01-19 Roussel Uclaf Procédé de préparation de composés cétoniques optiquement actifs et produits enrésultant
DD235394A3 (de) * 1968-08-30 1986-05-07 Barnikol Oettler Kurt Verfahren zur herstellung von oestradiol-3-methylaether
CA942670A (en) * 1969-07-28 1974-02-26 Richard A. Edgren Contraceptive compositions
ZA81348B (en) * 1980-01-30 1982-02-24 Akzo Nv Novel 17-amino-16-hydroxy steroids of the androstane and oestrane series and derivatives thereof,processes for their preparation and pharmaceutical compositions
US4330540A (en) * 1981-01-29 1982-05-18 Akzo N.V. Ent-16-amino-17-hydroxy-oestra-1,3,5(10)-trienes and derivatives thereof, and pharmaceutical compositions
EP0069424B1 (en) * 1981-07-07 1985-05-29 Akzo N.V. Process for the selective reduction of a 14, 17-dioxo-8,4-seco-steroid
FR2717690B1 (fr) * 1994-03-24 1996-04-26 Roussel Uclaf Application de stéroïdes aromatiques 3 substitués par un aminoalcoxy substitué à l'obtention d'un médicament pour contrôler la stérilité, notamment masculine.
FR2718138B1 (fr) * 1994-04-01 1996-04-26 Roussel Uclaf Nouveaux stéroïdes comportant en position 20 une chaîne aminosubstituée, procédé et intermédiaires de préparation, application comme médicaments et compositions pharmaceutiques les renfermant.

Also Published As

Publication number Publication date
ES2258005T3 (es) 2006-08-16
DE19917930A1 (de) 2000-10-19
AU4401100A (en) 2000-11-02
ATE316978T1 (de) 2006-02-15
CO5180552A1 (es) 2002-07-30
AR023497A1 (es) 2002-09-04
DE60025817D1 (de) 2006-04-13
EP1169336B1 (en) 2006-02-01
EP1169336A1 (en) 2002-01-09
WO2000063228A1 (en) 2000-10-26
DE60025817T2 (de) 2006-11-02
JP2002542255A (ja) 2002-12-10
PE20010042A1 (es) 2001-02-15

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Legal Events

Date Code Title Description
FZDE Discontinued